A copper-catalyzed system for the amidation of carboxylic acids with tert-amines through C–N bond cleavage was developed. This protocol is practical and represents a simple way to produce functionalized amides from basic starting materials in moderate to good yields. A plausible mechanism is proposed for the reaction.
PHENYL-CONTAINING N-ACYL AMINE AND AMINOACID DERIVATIVES, METHODS FOR THE PRODUCTION THEREOF, A PHARMACEUTICAL COMPOSITION AND THE USE THEREOF
申请人:Obschestvo S Ogranichennoi Otvetstennostiyu
"Pharmenterprises"
公开号:EP1876169A1
公开(公告)日:2008-01-09
The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-spasmodic actions, as well as capability to potentiate effect of other analgetics, and possessing in addition antihypoxic, antidepressant and anti-Parkinsonistic action; as well as to the processes for the preparation novel and known phenyl-N-acyl derivatives of biogenic amines, to a pharmaceutical composition and to an agent comprising compounds of general formula (I) as well as to use thereof and a method of treating.
A novel, efficient and environmentally friendly synthetic method has been developed for C(sp)-H selenation of arylacetamides with readily available diselenides as selenating reagents at room temperature. This protocol is applicable to a list of wide-ranging arylacetamides and diselenides, and provides various α-selenylated aryl amide derivatives with high yield using choline hydroxide (ChOH) as a green